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Brensocatib

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Chemical Structure| 1802148-05-5 同义名 : Azd7986;INS 1007;INS1007, Brensocatib
CAS号 : 1802148-05-5
货号 : A291759
分子式 : C23H24N4O4
纯度 : 99%+
分子量 : 420.461
MDL号 : MFCD31619232
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(249.73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Brensocatib acts as an inhibitor of DPP1, exhibiting pIC50 values of 6.85, 7.6, 7.7, 7.8, and 7.8 across various species—human, mouse, rat, dog, and rabbit, respectively. Brensocatib demonstrates stability in the propionaldehyde reactivity assay, maintaining a half-life exceeding 50 hours. When cells are differentiated in the presence of Brensocatib, ranging from 38 pM to 10 μM, a notable reduction in enzyme activity within cell lysates is observed for DPP1 and the three neutrophil serine proteases (NSPs)—NE, Pr3, and CatG. Brensocatib effectively suppresses the activation of these NSPs in a dose-responsive manner, with pIC50 values approximating 7 for each. At a concentration of 10 μM Brensocatib, the activity levels of NE, Pr3, and CatG are significantly diminished, dropping to 4 to 10% of the baseline control[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.89mL

2.38mL

1.19mL

23.78mL

4.76mL

2.38mL
参考文献

[1]Doyle K, et al. Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). J Med Chem. 2016 Oct 27;59(20):9457-9472.